abstract |
Compounds of a class of alkyl carboxy amino acid analogs of glutamic acid according to formula 1 act as specific regulators of kainic acid EAA receptor ca tion channel, wherein R1 is 1) CH3, or 2) halogen; R2 and R3 are independently 1) H, 2) C1-C6-alkyl, 3) C3-C4-alkenyl, 4) C3-C5-cycloalkyl, 5) C1-C6-alkyl-CO-, 6) C1-C6-alkyl-OCO-, 7) C1-C6-alkyl-NHCO-, 8) CHO-, or 9) C3-C6-alkynyl; R2 and R3 taken together can be -CH2(CH2)pCH2-; p is 0, 1, 2 or 3; and pharmaceutically acceptab le salts of these compounds, but not including compounds of Formula I wherein R2 an d R3 are H and R1 is CH3 or R1 is F. These compounds are useful for treating neurolog ical, neuropsychological, neuropsychiatric, neurodegenerative, neuropsychopharmacologi cal and functional disorders associated with excessive or insufficient activation of the kainic acid subtype of the ionotropic EAA recepto rs, treating cognitive disorders associated with deactivation, suboptimal activation or over-activation of the kainic acid receptor, alleviatin g pain and improving and enhancing memory, learning, and associated mental processes. A method for designing novel AMPA or kainic acid re ceptor agonists or antagonists is also disclosed. |